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Flashcards in Cancer Chemo Drugs Deck (25)
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Alkylating agents: cell cycle, MoA

cyclophosphamide, ifosphamide.
cell cycle non-specific
covalently bind alkyl group to DNA (N7 position of guanine) to inhibit DNA replication
and cause single and double stranded breaks and cross-linking.
Main side effect of cyclophosphamide and ifosfamide is hemorrhagic cystitis


What class is cyclophosphamide? What are the major side effects? Treatment of sides?

alkylating agent
side effect is hemorrhagic cystitis; cardiac toxicities at high doses
prevent hemorrhagic cystitis with MESNA rescue that binds the harmful metabolite


What class is ifosfamide? What are the main side effects and treatments? Treatment of sides?

alkylating agent
causes hemorrhagic cystitis
also has neurologic and nephrotoxicities
prevent hemorrhagic crisis with MESNA


What is cisplatin? (class) What are the major toxicities? Treatment of toxicities?

Platinum compound (acts similar to an alkylating agent)
Side effects include nausea (very significant)
Also significant nephrotoxicity and ototoxicity.
Try to prevent nephrotoxicity and ototoxicity with IV hydration, mannitol (promote excretion) and magnesium supplements


What is carboplatin?

Platinum compound (acts like an alkylating agent)
causes more myelosuppression and allergic reactions than cisplatin
causes less nephrotoxicity and ototoxicity


What are all the alkylating agents and alkylating-like agents I need to know (6)?

Pure alkylating:
1. cyclophosphamide
2. Ifofsimide
Platinum containing (alkylating-like agents):
3. cisplatin
4. carboplatin


What are antitumor antibiotics? (cell cycle, MOA)

derived from microbes
cell-cycle nonspecific
Kill via:
1. interacalation between base pairs
2. topoisomerase II inhibition (topoisomerase II is a DNA repair enzyme)
3. free radical generation leading to double and single stranded breaks.
4. Membrane disruption


What are the anthracyclines (class, examples)

class: antitumor antibiotics
example: doxorubicin, other -rubicin drugs


Doxorubicin: class, toxicity, treatment of toxicity

class: anthracyclines of the antitumor antibiotics
major toxicity is cardiac toxicity. try to prevent with dexrazoxane to bind free radicals


Bleomycin: class, toxicities

Bleomycin is a miscellaneous antitumor antibiotic used for Hodgkin's disease and germ cell tumors.
Bleomycin can cause pulmonary fibrosis.


What are antimetabolites? (cell cycle, MOA)

S phase specific
similar to metabolites in DNA/RNA synthesis pathways.
compete for key enzymes and/or become incorporated into DNA


What is methotrexate? class, toxicities

antimetabolite: folate antagonist
binds to dihydrofolate reductase and ultimately decreases DNA synthesis (prevents U --> T)
must give with rescue leucovorin that provides an alternate source of reduced folate to prevent deat of normal cells.
Side effects: mucositis, hepatotoxicity, at high doses: nephrotoxicity .


What factors must be specially considered with methotrexate?

genetic polymorphisms in the methylenetetrahydofolate reducase (MTHFR enzyme) that lead to increased senstivitiy to methotrexate toxicity.


What is cytarabine? (class) What toxicities are seen with cytarabine?

this is an antimetabolite and pyrimindine analogue. side effects include flu-like syndrome, cerebelar ataxia, and ocular probems (prevented with eyey drops).


What are vinca alkaloids?

drugs that inhibit microtubule assembly: mitotic inhibitor


What kind of drug is vincristine? What are side effects?

Vincristine is a vinca alkaloid that disrupts microtubule assembly
is is NON-myelosuppressive but does cause significant constipation and peripheral neuropathy. also causes skin irritation (less important)


What are taxanes?

mitotic inhibitor that stabilizes microtubules
(suffix: end in "taxel")


What are the classes of mitotic inhibitors?

vinca alkaloids and taxanes


What topoisomerase I inhibitor should I know? Cell cycle? What are its side effects?

Irinotecan (they all end in "ecan")
Side effects: GI tumors, diarrhea
S phase


What topoisomerase II inhibitors should I know? Cell cylce? Side effects?

Know etoposide
specific to S-G2 phase
cause allergic reactions
(it is also true that the antitumor antibiotics and the anthracyclines are are topoisomerase II inhbitors, but not given this way in lecture, grrrrrr).


Corticosteroids are used to treat some cancers. Which ones? Side effects?

treat lympoblastic leukemias, lymphomas
we don't know why they work/MoA
"good" side effects: anti-emetic, appetite stimulant
"bad" side effects surely exist, but I don't need to memorize them.


What kinds of hormone therapy are used in prostate cancer?

androgen deprivation, surgical or medical orchiectomy, anti-androgen drugs, estrogen


How is hormone therapy useful in breast cancer?

some breast cancers are estrogen positive and can be treated with tamoxifen, which is anti-estrogenic in breast tissue



MOA: depletes serum asparagine needed for protein synthesis by tumor cells. nornal cells can synthesize own asparagine.
Sides: hypersensitivity rxns (must have epipen ready).
also pancreatitis and hepatotoxicity
works better in peds pts



used in tx of multiple myeloma and some lymphomas.
sides: peripheral neuropathy, thrombocytopenia. given subcutaneously
26S proteosome inhibitor (protein regulation and homeostasis)